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Choc-Tadalafil Fusion: Unlocking Solubility and Taste Harmony with β-CD-Infused Medicated Chocolate. 巧克力-他达拉非融合:ß-CD浸泡药用巧克力的溶解性和口味和谐。
Pub Date : 2024-01-01 DOI: 10.2174/0126673878280254240312053406
Chetna Modi, Manobika Sinha, Vaishali Thakkar, Hardik Rana, Dipika Chavda

Objective: The primary limitations of tadalafil in treating erectile dysfunction are its low solubility and unpleasant bitter taste, which ultimately result in inadequate patient adherence. The present study aimed to develop and characterize a medicated chocolate formulation containing Tadalafil and β-CD (solubility enhancer) employing the concept of Design of Experiment (DoE) using chocolate as a user-friendly excipient.

Methods: An inclusion complex was formulated by incorporating the drug into β-CD using the kneading method for solubility improvement and also as a taste masker for Tadalafil. The ratio of drug: β-CD inclusion complex was selected based on a phase solubility study. The inclusion complex was molded into a chocolate base and optimized using the DoE approach. Further, drug excipient interaction was evaluated by DSC and FTIR study.

Results: Phase solubility study suggested a 1:1 ratio of Tadalafil: β-CD for better solubility. DSC spectra suggested the conversion of crystalline structure into an amorphous state which indicates improvement of the drug solubility. DSC and FTIR studies revealed that there was no significant interaction between drug and excipients. Next, %CDR (cumulative drug release) at 30 min revealed the immediate effect of Tadalafil from chocolate formulation and free drug analysis (an unbound drug with β-CD) proved reduced bitterness of the drug in the complex. Additionally, the medicated chocolate was found to be stable at room temperature as per stability study.

Conclusion: β-CD was found to be a promising multifunctional excipient as a solubility enhancement carrier and taste masker for bitter-tasting drugs.

目的:他达拉非在治疗勃起功能障碍方面的主要局限性在于其溶解度低和难闻的苦味,这最终导致了患者的依从性不足。本研究旨在利用实验设计(DoE)的概念,将巧克力作为一种方便使用的辅料,开发一种含有他达拉非和ß-CD(溶解度增强剂)的药用巧克力配方,并对其进行表征:方法:采用捏合法将药物加入ß-CD中,配制出一种包合物,以提高药物的溶解度,同时作为他达拉非的掩味剂。药物与ß-CD包合物的比例为ß-CD包合物的比例是根据相溶解度研究选定的。将包合物模塑到巧克力基底中,并采用 DoE 方法进行优化。此外,还通过 DSC 和 FTIR 研究评估了辅料与药物的相互作用:相溶性研究表明,塔达拉菲和 β-CD 的比例为 1:1,溶解性更好。DSC 光谱显示,结晶结构转变为无定形状态,这表明药物的溶解度有所提高。DSC 和傅立叶变换红外光谱研究表明,药物与辅料之间没有明显的相互作用。接下来,30 分钟的 %CDR(累积药物释放量)显示了巧克力配方中他达拉非的即时效果,游离药物分析(未与 ß-CD 结合的药物)证明了复合物中药物苦味的减少。结论:β-CD 是一种很有前途的多功能赋形剂,既能提高药物的溶解度,又能掩盖苦味药物的味道。
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引用次数: 0
Revolutionizing Brain Drug Delivery: Buccal Transferosomes on the Verge of a Breakthrough. 脑部给药革命:口腔转移体即将取得突破。
Pub Date : 2024-01-01 DOI: 10.2174/0126673878312336240802113811
Pavuluri Chandrasekhar, Rajaganapathy Kaliyaperumal

The buccal cavity, also known as the oral cavity, is a complex anatomical structure that plays a crucial role in various physiological processes. It serves as a gateway to the digestive system and facilitates the initial stages of food digestion and absorption. However, its significance extends beyond mere digestion as it presents a promising route for drug delivery, particularly to the brain. Transferosomes are lipid-based vesicles that have gained significant attention in the field of drug delivery due to their unique structure and properties. These vesicles are composed of phospholipids that form bilayer structures capable of encapsulating both hydrophilic and lipophilic drugs. Strategies for the development of buccal transferosomes for brain delivery have emerged as promising avenues for pharmaceutical research. This review aims to explore the various approaches and challenges associated with harnessing the potential of buccal transferosomes as a means of enhancing drug delivery to the brain. By understanding the structure and function of both buccal tissue and transferosomes, researchers can develop effective formulation methods and characterization techniques to optimize drug delivery. Furthermore, strategic approaches and success stories in buccal transferosome development are highlighted, showcasing inspiring examples that demonstrate their potential to revolutionize brain delivery.

颊腔又称口腔,是一个复杂的解剖结构,在各种生理过程中起着至关重要的作用。它是通往消化系统的门户,有助于食物消化和吸收的初始阶段。然而,口腔的意义远不止消化这么简单,它还是一条很有前景的药物输送途径,尤其是向大脑输送药物。转运体是一种基于脂质的囊泡,由于其独特的结构和特性,在药物递送领域备受关注。这些囊泡由磷脂组成,形成的双层结构能够包裹亲水性和亲油性药物。开发用于脑部给药的口腔转移体的策略已成为药物研究的一条大有可为的途径。本综述旨在探讨与利用口腔转移体的潜力作为加强向大脑给药的手段相关的各种方法和挑战。通过了解口腔组织和转移体的结构与功能,研究人员可以开发出有效的配制方法和表征技术,从而优化药物输送。此外,本书还重点介绍了开发口腔转移体的战略方法和成功案例,通过令人鼓舞的实例展示了口腔转移体彻底改变脑部给药方式的潜力。
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引用次数: 0
Technical Considerations, Applications, and Benefits of Organogels in Topical Drug Delivery Systems. 有机凝胶在局部给药系统中的技术考虑因素、应用和优势。
Pub Date : 2024-01-01 DOI: 10.2174/0126673878277455240214110033
Abhishek Yadav, Vikas Jhawat, Rahul Pratap Singh, Sunita Chauhan, Rohit Dutt, Rajesh Goyal, Deependra Singh

Organogels represent semi-solid systems where an organic liquid phase is entrapped within a three-dimensional network formed by self-assembled, crosslinked, or entangled gelator fibers. These versatile materials find applications in a wide range of fields, including chemistry, pharmaceuticals, cosmetics, biotechnology, and food technology. Notably, in pharmacology, they serve as valuable platforms for drug and vaccine delivery, facilitating the transport of active ingredients through various routes such as transdermal, oral, and parenteral. However, their previous utility as drug delivery systems was hindered by the toxicity associated with the organic solvents used. The pharmacokinetics of medications delivered via organogels are primarily influenced by the distinctive properties of these materials, specifically their "high permeability and poor aqueous solubility," which can impact the bioavailability of the drugs. Organogels can be employed topically or for the controlled release of medications through cutaneous administration and percutaneous absorption, expanding their scope of application beyond conventional drug delivery methods. Organogels hold significant promise as drug delivery vehicles due to their biocompatibility, non-irritating properties, and thermoremanent characteristics. They enable the formulation of diverse drug delivery systems by incorporating both hydrophilic and hydrophobic bioactive compounds within the gel matrix. This comprehensive review offers an overview of organogels, encompassing their nature, synthesis, characterization, and properties. Special attention is directed towards cutting-edge technologies employed in designing organogels as potential controlled delivery systems, with a focus on their emerging therapeutic applications.

有机凝胶是一种半固体体系,其中有机液相被包裹在由自组装、交联或缠结的凝胶体纤维形成的三维网络中。这些用途广泛的材料可应用于化学、制药、化妆品、生物技术和食品技术等多个领域。值得注意的是,在药理学领域,它们是药物和疫苗输送的重要平台,可通过透皮、口服和肠外等各种途径促进活性成分的输送。然而,由于所使用的有机溶剂具有毒性,阻碍了它们以前作为药物输送系统的实用性。通过有机凝胶给药的药代动力学主要受到这些材料独特性质的影响,特别是它们的 "高渗透性和低水溶性",这会影响药物的生物利用度。有机凝胶可用于局部给药或通过皮肤给药和经皮吸收控制药物释放,从而将其应用范围扩大到传统给药方法之外。有机凝胶具有生物相容性、无刺激性和热稳定性等特点,因此很有希望成为一种给药载体。通过在凝胶基质中加入亲水性和疏水性生物活性化合物,它们可以配制出多种给药系统。本综述概述了有机凝胶的性质、合成、表征和特性。文章特别关注了将有机凝胶设计为潜在控制给药系统的前沿技术,并重点介绍了有机凝胶的新兴治疗应用。
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引用次数: 0
A Comprehensive Review on Potential Chemical and Herbal Permeation Enhancers Used in Transdermal Drug Delivery Systems. 全面回顾透皮给药系统中使用的潜在化学和草药渗透促进剂。
Pub Date : 2024-01-01 DOI: 10.2174/0126673878272043240114123908
Rajat Singh Raghav, Sushma Verma, Monika

Using skin patches to deliver drugs is dependable and doesn't have the same issues as permeation enhancers, which help drugs get through the skin but struggle because of the skin's natural barrier. Strategies are required to increase topical bioavailability to enhance drug absorption. Natural compounds offer a promising solution by temporarily reducing skin barrier resistance and improving drug absorption. Natural substances allow a wider variety of medications to be distributed through the stratum corneum, offering a dependable approach to enhancing transdermal drug delivery. Natural substances have distinct advantages as permeability enhancers. They are pharmacologically effective and safe, inactive, non-allergenic, and non-irritating. These characteristics ensure their suitability for use without causing adverse effects. Natural compounds are readily available and well tolerated by the body. Studies investigating the structure-activity relationship of natural chemicals have demonstrated significant enhancer effects. By understanding the connection between chemical composition and enhancer activity, researchers can identify effective natural compounds for improving drug penetration. In conclusion, current research focuses on utilizing natural compounds as permeability enhancers in transdermal therapy systems. These substances offer safety, non-toxicity, pharmacological inactivity, and non-irritation. Through structure-activity relationship investigations, promising advancements have been made in enhancing drug delivery. Using natural compounds holds enormous potential for improving the penetration of trans-dermally delivered medications.

使用皮肤贴剂给药是可靠的,而且不像渗透增强剂那样存在问题,渗透增强剂有助于药物通过皮肤,但由于皮肤的天然屏障,药物很难通过皮肤。我们需要采取策略来提高局部生物利用度,从而促进药物的吸收。天然化合物能暂时降低皮肤屏障的阻力,促进药物吸收,是一种很有前景的解决方案。天然物质可使更多种类的药物通过角质层分布,为加强透皮给药提供了可靠的方法。天然物质作为渗透性增强剂具有明显的优势。它们在药理上有效、安全、无活性、无过敏性、无刺激性。这些特点确保了它们在使用时不会产生不良影响。天然化合物容易获得,人体耐受性好。对天然化学物质结构与活性关系的研究表明,天然化学物质具有显著的增效作用。通过了解化学成分与增强剂活性之间的关系,研究人员可以找到有效的天然化合物来提高药物渗透性。总之,目前的研究重点是在透皮治疗系统中利用天然化合物作为渗透性增强剂。这些物质具有安全、无毒、无药理活性和无刺激等特点。通过结构-活性关系研究,在增强药物输送方面取得了可喜的进展。利用天然化合物提高透皮给药的渗透性具有巨大的潜力。
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引用次数: 0
Design, Development and In-Vitro Characterization of Insulin Loaded Topical Pluronic-Lecithin Based Organogel Formulation for the Management of Diabetic Wound. 设计、开发和体外表征用于治疗糖尿病伤口的胰岛素外用聚uronic-卵磷脂有机凝胶配方
Pub Date : 2024-01-01 DOI: 10.2174/0126673878279693231227081931
Sunita Chauhan, Vikas Jhawat, Rahul Pratap Singh, Abhishek Yadav, Vandana Garg

Aim: To develop and characterize the topical insulin-loaded organogel formulation for the management of diabetic wounds.

Objectives: To formulate and evaluate organogel of insulin that can serve as a topical administration for promoting enhanced wound healing in diabetic patients by providing sustained and localized delivery of drug to the wound site.

Methodology: The insulin organogel formulated by the micro-emulsion method involves mixing the "aqueous and oil phases" at high shear. Physical and chemical properties, as well as an in vitro study with a Franz diffusion chamber, were used to evaluate the prepared organogel.

Results: All formulations proved to be off-white, homogeneous, washable, and had a pH between 6 and 6.5; moreover, they were non-irritating and skin-compatible. Formulations F1-F6 had viscosity ranging from 2058 to 3168 cps, spreadability ranges of 0.35 to 0.52 g*cm/s, and gel transition ranges of 28.33 to 35.33 °C. In formulations F1-F3, the concentration of lecithin was gradually increased, and in formulations F4-F6, the concentration of PF-127 was increased, resulting in a decrease in gel transition temperature, an increase in viscosity, and a gradual change in spreadability. The higher-viscosity formulations were much more stable and had better drug release. All formulations were fitted to a kinetic model belonging to first-order kinetics. However, after examining the parameter evaluation, it was found that the formulations F2 and F6 were better suited to the kinetic model and were consistent with the first-order and Higuchi models in Korsmeyer-Peppas F2 (r2 = 0.9544 and n = 1.0412); F6 (r2 = 0.9019 and n = 1.0822), which was a confirmation of the sustainability of the release system with matrix diffusion and drug delivery mechanisms that were based on the Super-Case II transport.

Conclusion: Further research and clinical trials are needed to validate its efficacy, optimize the formulation, and establish its long-term safety. Topical insulin organogel has the potential to revolutionize diabetic wound management by improving healing outcomes, reducing complications, and raising the standard of living for those who have diabetes.

目的:开发并鉴定用于治疗糖尿病伤口的局部胰岛素有机凝胶配方:配制和评估胰岛素有机凝胶,通过向伤口部位持续局部给药,促进糖尿病患者伤口愈合:胰岛素有机凝胶采用微乳液法配制,包括在高剪切下混合 "水相和油相"。方法:采用微乳液法配制的胰岛素有机凝胶需要在高剪切力下混合 "水相和油相",并利用物理和化学特性以及弗朗兹扩散室的体外研究对配制的有机凝胶进行评估:结果:所有配方均为灰白色,均匀,可清洗,pH 值介于 6 和 6.5 之间;此外,它们无刺激性,与皮肤相容。配方 F1-F6 的粘度范围为 2058 至 3168 cps,铺展性范围为 0.35 至 0.52 g*cm/s,凝胶转变范围为 28.33 至 35.33 °C。在配方 F1-F3 中,卵磷脂的浓度逐渐增加,而在配方 F4-F6 中,PF-127 的浓度增加,导致凝胶转变温度降低,粘度增加,铺展性逐渐改变。粘度较高的配方更加稳定,药物释放效果更好。所有配方均符合一阶动力学模型。然而,在对参数进行评估后发现,配方 F2 和 F6 更适合动力学模型,与 Korsmeyer-Peppas 的一阶模型和 Higuchi 模型一致 F2(r2 = 0.9544,n = 1.0412);F6(r2 = 0.9019,n = 1.0822),这证实了基质扩散释放系统的可持续性和基于超基质 II 转运的给药机制:结论:还需要进一步的研究和临床试验来验证其疗效、优化配方并确定其长期安全性。外用胰岛素有机凝胶有望通过改善愈合效果、减少并发症和提高糖尿病患者的生活水平,彻底改变糖尿病伤口的管理。
{"title":"Design, Development and <i>In-Vitro</i> Characterization of Insulin Loaded Topical Pluronic-Lecithin Based Organogel Formulation for the Management of Diabetic Wound.","authors":"Sunita Chauhan, Vikas Jhawat, Rahul Pratap Singh, Abhishek Yadav, Vandana Garg","doi":"10.2174/0126673878279693231227081931","DOIUrl":"10.2174/0126673878279693231227081931","url":null,"abstract":"<p><strong>Aim: </strong>To develop and characterize the topical insulin-loaded organogel formulation for the management of diabetic wounds.</p><p><strong>Objectives: </strong>To formulate and evaluate organogel of insulin that can serve as a topical administration for promoting enhanced wound healing in diabetic patients by providing sustained and localized delivery of drug to the wound site.</p><p><strong>Methodology: </strong>The insulin organogel formulated by the micro-emulsion method involves mixing the \"aqueous and oil phases\" at high shear. Physical and chemical properties, as well as an in vitro study with a Franz diffusion chamber, were used to evaluate the prepared organogel.</p><p><strong>Results: </strong>All formulations proved to be off-white, homogeneous, washable, and had a pH between 6 and 6.5; moreover, they were non-irritating and skin-compatible. Formulations F1-F6 had viscosity ranging from 2058 to 3168 cps, spreadability ranges of 0.35 to 0.52 g*cm/s, and gel transition ranges of 28.33 to 35.33 °C. In formulations F1-F3, the concentration of lecithin was gradually increased, and in formulations F4-F6, the concentration of PF-127 was increased, resulting in a decrease in gel transition temperature, an increase in viscosity, and a gradual change in spreadability. The higher-viscosity formulations were much more stable and had better drug release. All formulations were fitted to a kinetic model belonging to first-order kinetics. However, after examining the parameter evaluation, it was found that the formulations F2 and F6 were better suited to the kinetic model and were consistent with the first-order and Higuchi models in Korsmeyer-Peppas F2 (r2 = 0.9544 and n = 1.0412); F6 (r2 = 0.9019 and n = 1.0822), which was a confirmation of the sustainability of the release system with matrix diffusion and drug delivery mechanisms that were based on the Super-Case II transport.</p><p><strong>Conclusion: </strong>Further research and clinical trials are needed to validate its efficacy, optimize the formulation, and establish its long-term safety. Topical insulin organogel has the potential to revolutionize diabetic wound management by improving healing outcomes, reducing complications, and raising the standard of living for those who have diabetes.</p>","PeriodicalId":94352,"journal":{"name":"Recent advances in drug delivery and formulation","volume":" ","pages":"50-60"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139571788","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ion-activated In Situ Gel of Gellan Gum Containing Chrysin for Nasal Administration in Parkinson's Disease. 含黄豆素结冷胶的离子激活原位凝胶用于帕金森病鼻给药。
Pub Date : 2024-01-01 DOI: 10.2174/0126673878279656231204103855
Khushboo Lavania, Anuj Garg

Introduction: This study focused on creating an innovative treatment approach for Parkinson's disease (PD), a progressive neurodegenerative condition characterized by the loss of specific neurons in the brain.

Aim: The research aimed to develop a nasal gel using gellan gum containing a complex of chrysin with hydroxypropyl-β-cyclodextrin (HP-β-CD) to enhance the drug's solubility and stability.

Method: The formulation process involved utilizing central composite design (CCD) to optimize the concentrations of gellan gum and HPMC E5, with viscosity and mucoadhesive strength as key factors. The resulting optimized In Situ gel comprised 0.7% w/v gellan gum and 0.6% w/v HPMC E5, exhibiting desirable viscosity levels for both sol and gel states, along with robust mucoadhesive properties. The formulated gel underwent comprehensive evaluation, including assessments for gelation, drug content, in vitro drug release, ex vivo permeation, and histopathology.

Result: The findings demonstrated superior drug release from the In Situ gel compared to standalone chrysin. Ex vivo studies revealed effective drug permeation through nasal mucosa without causing harm. Moreover, experiments on neuronal cells exposed to oxidative stress (H2O2- induced) showcased significant neuroprotection conferred by chrysin and its formulations. These treatments exhibited notable enhancements in cell viability and reduced instances of apoptosis and necrosis, compared to the control group. The formulations exhibited neuroprotective properties by mitigating oxidative damage through mechanisms, like free radical scavenging and restoration of antioxidant enzyme activity.

Conclusion: In conclusion, this developed In situ gel formulation presents a promising novel nasal delivery system for PD therapy. By addressing challenges related to drug properties and administration route, it holds the potential to enhance treatment outcomes and improve the quality of life for individuals with Parkinson's disease.

本研究的重点是为帕金森病(PD)创造一种创新的治疗方法,帕金森病是一种进行性神经退行性疾病,其特征是大脑中特定神经元的丧失。目的:制备含大黄素-羟丙基-β-环糊精(HP-β-CD)复合物的结冷胶鼻用凝胶,以提高药物的溶解度和稳定性。方法:以黏度和粘接强度为主要因素,采用中心复合设计(CCD)对结冷胶和HPMC E5的浓度进行优化。优化后的原位凝胶由0.7% w/v的结冷胶和0.6% w/v的HPMC E5组成,在溶胶和凝胶状态下都表现出理想的粘度水平,以及强大的粘接性能。对配制的凝胶进行综合评价,包括凝胶性、药物含量、体外药物释放、体外渗透和组织病理学评估。结果:原位凝胶的释药效果优于单独的白菊花素。体外研究表明,药物可通过鼻黏膜有效渗透而无损伤。此外,对暴露于氧化应激(H2O2诱导)的神经细胞的实验显示,菊花素及其配方具有显著的神经保护作用。与对照组相比,这些治疗明显增强了细胞活力,减少了细胞凋亡和坏死的发生。该配方通过清除自由基和恢复抗氧化酶活性等机制减轻氧化损伤,显示出神经保护特性。结论:这种原位凝胶制剂是一种很有前景的PD治疗鼻腔给药系统。通过解决与药物特性和给药途径相关的挑战,它具有增强治疗效果和改善帕金森病患者生活质量的潜力。
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引用次数: 0
Robotic Pills as Innovative Personalized Medicine Tools: A Mini Review 作为创新型个性化医疗工具的机器人药片:微型综述
Pub Date : 2023-12-15 DOI: 10.2174/0126673878265457231205114925
Komal Rane, Garima Kukreja, Siddhi Deshmukh, Urmisha Kakad, Pranali Jadhav, Vinita Pawar
The most common route for drug administration is the oral route due to the various advantages offered by this route, such as ease of administration, controlled and sustained drug delivery, convenience, and non-invasiveness. In spite of this, oral drug absorption faces challenges dueto various issues related to its stability, permeability and solubility in the GI tract. Biologic drugsgenerally face problems when administered by oral route as they are readily degradable and thus required to be injected. To overcome these issues in oral absorption, different approaches like noveldrug delivery systems and newer pharmaceutical technologies have been adopted. With a combinedknowledge of drug delivery and pharmaceutical technology, robotic pills can be designed and usedsuccessfully to enhance the adhesion and permeation of drugs through the mucus membrane of theGI tract to achieve drug delivery at the target site. The potential application of robotic pills in diagnosis and drug dispensing is also discussed. The review highlights recent developments in roboticpill drug-device technology and discusses its potential applications to solve the problems and challenges in oral drug delivery.
最常见的给药途径是口服途径,因为这种途径具有各种优势,如易于给药、可控和持续给药、方便和无创。尽管如此,口服药物的吸收仍面临着各种挑战,包括药物在消化道中的稳定性、渗透性和溶解性等问题。生物药在口服途径给药时通常会遇到一些问题,因为它们很容易降解,因此需要注射。为了克服这些口服吸收问题,人们采用了不同的方法,如新型给药系统和较新的制药技术。结合给药和制药技术的知识,可以设计并成功使用机器人药丸来增强药物在胃肠道粘膜上的粘附力和渗透力,从而实现在目标部位给药。此外,还讨论了机器人药丸在诊断和配药方面的潜在应用。综述重点介绍了机器人药丸药物装置技术的最新发展,并讨论了其在解决口服给药问题和挑战方面的潜在应用。
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引用次数: 0
Development of Niosomal Vesicles Loaded Mometasone Furoate Gel for Transdermal Delivery and its Evaluation. 膜小体载糠酸莫米松凝胶经皮给药的研制及其评价。
Pub Date : 2023-01-01 DOI: 10.2174/0126673878259437231031114907
Bhushan R Rane, Pushkar Y Chavan, Nidhi S Kate, Ashish S Jain

Background: Mometasone Furoate (MF) is a corticosteroid (glucocorticoid) used to treat eczema, psoriasis, allergies, and rash on the skin; also used to reduce itching, redness, and swelling (inflammation). It has been reported that the bioavailability of MF is less than 11% when given via the nasal route. Encapsulating the drug in niosomes can improve the active pharmaceutical ingredient's bioavailability by enhancing both physical and biological stability.

Objective: The goal of the study is to develop, a non-ionic surfactant-based vesicular system, by loading mometasone furoate, and introducing it into a gel-based formulation by utilizing an appropriate gelling agent, and performing its evaluation.

Methods: The niosome vesicle was prepared by vacuum rotary evaporation method (Thin film hydration method). Gel was prepared using the dispersion method and in-vitro drug diffusion studies using Franz-diffusion cells.

Results: According to the results of the experiments conducted for the study, Mometasone Furoate niosomal gel was prepared utilizing Mometasone Furoate niosomes that were made using the thin film hydration process, Cholesterol, and Span 60, and loaded in various amounts of Carbopol as a geling agent. The niosomes' zeta potential was found to be -24 mV, showing that the formulation is stable. The polydispersity index (PDI) was found to be 0.409 and the average size of niosomes to be 252.7 nm. The performance of the gel of the optimized formulations containing 2% Carbopol showed in vitro diffusion for 7 hours and an increased flux rate as compared to the plain MF.

Conclusion: The experiments carried out during the study led to the conclusion that the thin-film hydration method was suitable for the formation of the MF-niosomes by using Span 60 and Cholesterol (2:1). The gel formulation containing 2% Carbopol indicated better in vitro diffusion following the Higuchi model across all niosomal gel formulations. Niosomal gel can be regarded as the best vesicular carrier for the efficient distribution of mometasone furoate via the transdermal route.

背景:糠酸莫米松(MF)是一种皮质类固醇(糖皮质激素),用于治疗湿疹、牛皮癣、过敏和皮肤皮疹;也用于减轻瘙痒、红肿(炎症)。据报道,经鼻给药时,MF的生物利用度低于11%。将药物包埋在纳米体中可以通过提高药物的物理和生物稳定性来提高活性药物成分的生物利用度。目的:本研究的目的是通过负载糠酸莫米松,并通过适当的胶凝剂将其引入凝胶基配方,并对其进行评估,从而开发一种非离子表面活性剂为基础的囊泡系统。方法:采用真空旋转蒸发法(薄膜水化法)制备膜小体囊泡。凝胶采用分散法制备,体外弗兰兹扩散细胞进行药物扩散研究。结果:根据本研究的实验结果,采用薄膜水合工艺、胆固醇、Span 60制备糠酸莫米松乳质体,并以不同量的卡波醇为胶凝剂,制备糠酸莫米松乳质体凝胶。纳米体的zeta电位为-24 mV,表明该制剂是稳定的。多分散性指数(PDI)为0.409,粒体的平均尺寸为252.7 nm。结果表明,含2%卡波波尔的优化配方凝胶的体外扩散时间为7小时,通量比普通MF增加。结论:本研究中所进行的实验表明,以Span 60和胆固醇(2:1)为原料,薄膜水化法适用于MF-niosomes的形成。根据Higuchi模型,含有2%卡波波尔的凝胶制剂在所有乳质体凝胶制剂中具有更好的体外扩散。乳质体凝胶是糠酸莫米松经皮有效分布的最佳囊泡载体。
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引用次数: 0
Pharmaceutical Suspensions: An Updated Patent Review on Novel Suspending Agents and Recent Advancement. 药物悬浮液:新型悬浮剂专利综述及最新进展。
Pub Date : 2023-01-01 DOI: 10.2174/0126673878246149231010085610
Prince Kumar, Madhu Verma

A wide variety of dosage forms are used for the oral administration of drugs to humans and animals. Apart from solid dosage forms, it also includes liquid dosage forms, such as solutions, suspensions, and emulsions. The selection is based on the physiochemical attributes of the therapeutically active ingredient. Suspensions are classified as dispersed systems that are heterogeneous in nature and consist of two phases. One phase is the continuous phase, the dispersion medium, or the external phase, which is either liquid or semisolid; the other is a solid particle dispersed in the external phase and called an internal or dispersed phase. They have several advantages over other dosage forms, such as effectively delivering hydrophobic drugs, avoiding the need for cosolvents, masking unpleasant tastes, and providing resistance to degradation and easy swallowing for young or elderly patients. They also attain higher drug concentrations compared to solution forms. This review article aims to study and explore the advantages, novel suspending agents, patent preference, and innovations of pharmaceutical suspension. It was targeted to scrutinize the literature floating in the internet domain regarding pharmaceutical suspension for delivery of drugs by oral route. The literature survey is targeted at the novel herbal suspending agents used, their patents involved, and innovations in the dosage form. Further, the study gives an insight into various aspects of suspension, such as classification of suspension, theories of suspension, various components used in suspension formulation, formulation aspect of suspension, evaluation parameters of suspension, patents, innovations, and regulatory status.

各种各样的剂型用于给人和动物口服药物。除固体剂型外,还包括液体剂型,如溶液、悬浮液和乳剂。选择是基于治疗活性成分的物理化学属性。悬浮液被归类为分散的系统,本质上是异质的,由两相组成。一相为连续相、分散介质或外相,为液体或半固体;另一种是分散在外相中的固体颗粒,称为内相或分散相。与其他剂型相比,它们有几个优点,例如有效地递送疏水药物,避免对共溶剂的需要,掩盖令人不快的味道,并且对年轻或老年患者具有抗降解和易于吞咽的能力。与溶液形式相比,它们也获得更高的药物浓度。本文旨在研究和探讨药物悬浮液的优点、新型悬浮剂、专利偏好和创新。目的是仔细审查漂浮在互联网领域的关于药物悬浮液口服给药的文献。文献调查是针对新型草药悬浮剂的使用,他们的专利涉及,并在剂型创新。进一步深入了解悬液的分类、悬液理论、悬液配方中使用的各种成分、悬液配方方面、悬液评价参数、专利、创新、监管现状等悬液的各个方面。
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引用次数: 0
Gum-based Nanoparticles Targeting for Colon Rectal Cancer: Latest Research and Patents. 靶向癌症的口香糖纳米粒子:最新研究和专利。
Pub Date : 2023-01-01 DOI: 10.2174/0126673878242191231017095804
Shilpi Shakya, Ritesh Kumar Tiwari, Arti Gupta

Colorectal disease is the third most prevelant cancer in both men and women, with an expected 106,180 new cases of colon cancer and 44,850 new cases of rectal cancer as per American Cancer Society. Targeted medicine delivery is vital in the treatment of colon disorders because it delivers long-term therapeutic results with little side effects. Natural polymer is biocompatible and biodegradable, which enables safety, improves storage, and physiological stability, it is utilized as drug delivery vehicles and has made great strides in recent years. Chitosan, alginate, pectin, guar gum, dextran, hyaluronic acid, and arabinoxylan are examples of natural polysaccharides that are utilized to create nanoparticles. Natural gums serve two purposes: first, they shield the medicine from stomach and intestinal conditions, allowing it to only be released in the colon. In this review, we introduce the different gum particularly used in nanoparticles formulation, and then discuss recent research and the latest patent in the development of gum-based nanoparticles for the treatment of colon rectal cancer.

结直肠癌是男性和女性中发病率第三高的癌症,根据美国癌症协会的数据,预计癌症新增病例106180例,癌症新增病例44850例。靶向给药在结肠疾病的治疗中至关重要,因为它能带来长期的治疗效果,几乎没有副作用。天然聚合物具有生物相容性和生物可降解性,具有安全性、改善储存和生理稳定性,被用作药物递送载体,近年来取得了长足进步。壳聚糖、藻酸盐、果胶、瓜尔胶、右旋糖酐、透明质酸和阿拉伯木聚糖是用于制造纳米颗粒的天然多糖的例子。天然牙龈有两个用途:首先,它们保护药物免受胃肠道疾病的影响,使其只能在结肠中释放。在这篇综述中,我们介绍了不同的口香糖,特别是用于纳米颗粒配方,然后讨论了最近的研究和最新的专利在开发用于治疗结直肠癌癌症的口香糖纳米颗粒。
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引用次数: 0
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Recent advances in drug delivery and formulation
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